N-Acetylation of p-Aminosalicylic Acid Derivatives by Black Aspergilli

Failure of P-(di-n-propylsulfamyl)-benzoic acid (benemid) to influence p-aminosalicylic acid blood levels.

Inhibitory effect of flavonoids on N-acetylation of 5-aminosalicylic acid in cultured rat hepatocytes.

5-Aminosalicylic acid (5-ASA) is an effective drug for the treatment of ulcerative colitis and Crohn's disease. A large group of flavonoids was investigated for their inhibitory effects on the N-acetyl-conjugation of 5-ASA in rat hepatocytes and subcellular preparations. When added to cultured hepatocytes, some flavonoids inhibited the production of N-acetyl-5-aminosalicylic acid (5-AcASA) with...

Mechanism of competitive inhibition of p-aminobenzoic acid oxidation by p-aminosalicylic acid.

The proposed mechanism(s) associated with the inhibition of essential metabolic reactions by various compounds has received a great deal of attention in recent years, since antimetabolites have proved useful in several chemotherapeutic areas and in studying various metabolic reactions. The significance of p-aminobenzoic acid in microbial nutrition was first emphasized when Woods (1940) and Wood...

Partial purification and properties of the isoniazid transacetylase in human liver. Its relationship to the acetylation of p-aminosalicylic acid.

The heritable trait of rapid and slow inactivation of isoniazid (isonicotinic acid hydrazide) in man is a topic of considerable interest in the developing field of pharmacogenetics (1). Although differences in acetylation appear to be the principal reason for inactivation differences, knowledge of the specific enzymic basis as well as of the relationship of this trait to the acetylation of chem...

Identification and functional characterization of arylamine N-acetyltransferases in eubacteria: evidence for highly selective acetylation of 5-aminosalicylic acid.

Arylamine N-acetyltransferase activity has been described in various bacterial species. Bacterial N-acetyltransferases, including those from bacteria of the gut flora, may be involved in the metabolism of xenobiotics, thereby exerting physiopathological effects. We characterized these enzymes further by steady-state kinetics, time-dependent inhibition, and DNA hybridization in 40 species, mostl...